PPAR-activating compound and pharmaceutical composition comprising the compound

Abstract

A compound represented by the following formula (1): Or a salt thereof; and therapeutic durgs containing the compound. The compound selectively activates PPARα.

1. A compound represented by the following formula (1): 
       
         
           
           
               
               
           
         
       
       wherein each of R 1  and R 2 , which may be identical to or different from each other, represents hydrogen, methyl, or ethyl; each of R 3a , R 3b , R 4a , and R 4b , which may be identical to or different from each other, represents hydrogen, halogen, nitro, hydroxyl, C 1-4  alkyl, trifluoromethyl, C 1-4  alkoxy, C 1-4  alkylcarbonyloxy, di-C 1-4  alkylamino, C 1-4  alkylsulfonyloxy, C 1-4  alkylsulfonyl, C 1-4  alkylsulfinyl, or C 1-4  alkylthio, or R 3a  and R 3b , or R 4a  and R 4b  optionally are linked together to form an alkylenedioxy group; X represents oxygen, sulfur or N—R 5 , wherein R 5  represents hydrogen, C 1-4  alkyl, C 1-4  alkylsulfonyl, or C 1-4  alkyloxycarbonyl group; Y represents oxygen, S(O) 1 , wherein 1 is 0,1 or 2, carbonyl, carbonylamino, aminocarbonyl, sulfonylamino, aminosulfonyl, or NH; n is a number from 1 to 6; and m is a number from 2 to 6, or a salt thereof. 
     
     
       2. The compound according to  claim 1 , wherein X and Y represent oxygen. 
     
     
       3. A compound selected from the group consisting of 2-[3-[[N-(Benzoxazol-2-yl)-N-3-(4-fluorophenoxy)propyl]aminomethyl]phenoxy]butyric acid, 2-[3-[[N-(Benzoxazol-2-yl)-N-2-(4-chlorophenoxy)ethyl]aminomethyl]phenoxy]butyric acid, 2-[3-[[N-(Benzoxazol-2-yl)-N-2-(4-chlorophenoxy)ethyl]aminomethyl]phenoxy]butyric acid, 
       2-[3-[[N-(Benzoxazol-2-yl)-N-3-phenoxypropyl]aminomethyl]phenoxy]propionic acid, 2-[3-[[N-(Benzoxazol-2-yl)-N-3-phenoxypropyl]aminomethyl]phenoxy]acetic acid, 2-[3-[[N-(Benzoxazol-2-yl)-N-3-phenoxypropyl]aminomethyl]phenoxy]butyric acid, 2-[3-[[N-(Benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy]butyric acid, 
       2-[3-[[N-(Benzoxazol-2-yl)-N-3-(4-methoxyphenoxy)propyl]aminomethyl]phenoxy]propionic acid and a salt thereof. 
     
     
       4. A pharmaceutical composition comprising a compound or a salt thereof as recited in  claim 1 ,  2  or  3  and a pharmacologically acceptable carrier. 
     
     
       5. A method for treating pathological conditions selected from the group consisting of hyperlipidemia, arteriosclerosis, diabetes, complications of diabetes, and inflammation comprising:
 administering to a subject in need thereof an effective amount of a compound or a salt thereof as recited in  claim 1 ,  2  or  3 .